17 research outputs found
Effect of the characteristics of raw material ibuprofen on roller compaction and dissolution
No full textThe Amorphous Quercetin/ Hydroxypropylmethylcellulose Acetate Succinate Solid Dispersions Prepared by Co-Precipitation Method to Enhance Quercetin Dissolution
No full text“Felodipine-indomethacin” co-amorphous supersaturating drug delivery systems: “Spring-parachute” process, stability, in vivo bioavailability, and underlying molecular mechanisms
No full textThe inhibiting role of hydroxypropylmethylcellulose acetate succinate on piperine crystallization to enhance its dissolution from its amorphous solid dispersion and permeability
No full text
In vitro and in vivo assessment of hydroxypropyl cellulose as functional additive for enabling formulations containing itraconazole
No full textEffect of Temperature and Moisture on the Physical Stability of Binary and Ternary Amorphous Solid Dispersions of Celecoxib
No full textUnivariate and Multivariate Models for Determination of Prasugrel Base in the Formulation of Prasugrel Hydrochloride Using XRPD Method
No full text
Improved Stability of Proline-Derived Direct Thrombin Inhibitors through Hydroxyl to Heterocycle Replacement
No full textModification
of the previously disclosed (<i>S</i>)-<i>N</i>-(2-(aminomethyl)-5-chlorobenzyl)-1-((<i>R</i>)-2-hydroxy-3,3-dimethylbutanoyl)pyrrolidine-2-carboxamide <b>2</b> by optimization of the P3 group afforded novel, low molecular
weight thrombin inhibitors. Heterocycle replacement of the hydroxyl
functional group helped maintain thrombin<i> in vitro</i> potency while improving the chemical stability and pharmacokinetic
profile. These modifications led to the identification of compound <b>10</b>, which showed excellent selectivity over related serine
proteases as well as <i>in vivo</i> efficacy in the rat
arteriovenous shunt. Compound <b>10</b> exhibited significantly
improved chemical stability and pharmacokinetic properties over <b>2</b> and may be utilized as a structurally differentiated preclinical
tool comparator to dabigatran etexilate (<b>Pro-1</b>) to interrogate
the on- and off-target effects of oral direct thrombin inhibitors
